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Assay Detail

CHEMBL748802

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding activity against muscarinic receptor in rat brain using [3H]QNB as the radioligand
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Muscarinic acetylcholine receptor (CHEMBL1907609)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Sterically hindered 5,11-dicarbo analogues of clozapine as potential chiral antipsychotic agents.
Rupard JH, de Paulis T, Janowsky A, Smith HE.
J Med Chem (1989) 32 : 2261 -2268
PubMed 2571728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.32 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73538 1 7.41
CHEMBL42 CLOZAPINE 4.0 1 7.29
CHEMBL415300 ISOCLOZAPINE 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73538 IC50 = 39.0 nM 7.41
CHEMBL42 CLOZAPINE IC50 = 51.0 nM 7.29
CHEMBL415300 ISOCLOZAPINE IC50 = 55.0 nM 7.26